Academic literature on the topic 'Sustained Release Formulations'

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Journal articles on the topic "Sustained Release Formulations"

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Mandhan, Rahul, and Twinkle Garg. "Sustained Release Matrix Technology for Cefixime- A Review." International Journal of Pharmaceutical Sciences and Medicine 7, no. 8 (2022): 10–19. http://dx.doi.org/10.47760/ijpsm.2022.v07i08.002.

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Sustained release drug delivery system is designed to sustain the release of the drug dosage forms at a predetermined rate. Sustained release formulation maintains uniform drug level in therapeutic window, improved efficacy of drug by localization at the site of action with better patient compliance, reducing the dose required, providing uniform drug delivery. The sustained release formulations minimize the frequency of drug administration and do not interfere with the therapeutic action of the drug. The use of sustained release matrix technology for antibiotics is effective in preventing the resistant of antibiotics in body on irrational use. Drug release through matrix SRDDS is determined by Polymer swelling, Water penetration, Drug dissolution, diffusion, Matrix erosion. The present article contains brief review on various formulation approaches for Sustained release drug delivery system, advantages, selection criteria for matrix SRDDS and use of cefixime trihydrate in formulating matrix SRDDS.
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Murdoch, David, and Rex N. Brogden. "Sustained Release Nifedipine Formulations." Drugs 41, no. 5 (1991): 737–79. http://dx.doi.org/10.2165/00003495-199141050-00006.

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Karim, Samira, Mohiuddin Ahmed Bhuiyan, and Md Sohel Rana. "Formulation and in vitro Evaluation of Glimepiride Sustained Release Tablets: Comparison with Immediate Release Tablets." Bangladesh Pharmaceutical Journal 18, no. 2 (2015): 157–62. http://dx.doi.org/10.3329/bpj.v18i2.24315.

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This work aims at the design of a sustained release formulation of glimepiride which is currently available in the treatment of type 2 diabetes mellitus and to investigate the effect of polymers on the release profile of glimepiride. Glimepiride sustained release tablets were prepared by direct compression method using different ratios of various release retarding polymers such as carbopol, ethyl cellulose, methocel K4 MCR, methocel K15 MCR, methocel K100 MCR and xanthum gum. These formulations were also compared with glimepiride immediate release tablets. The prepared tablets were subjected to various physical parameter tests including weight variation, friability, hardness, thickness, diameter, etc. In vitro dissolution studies of the formulations were done at pH 6.8 in phosphate buffer using USP apparatus 2 (paddle method) at 50 rpm. The percent releases of all the formulations (30) were 73.11%- 98.76% after 8 hours. The release pattern followed zero order kinetics and the release of the drug was hindered by the polymers used in the study. On the other hand, 100% drug was released within 1 hour from the immediate release tablet of glimepiride. The study reveals that the polymers used have the capacity to retard the release of the drug from the sustained release tablets and the more is the amount of the polymer in the formulation the less is the release of drug showing more retardation of drug release.Bangladesh Pharmaceutical Journal 18(2): 157-162, 2015
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Simran, Tanwar, Tikariya Komal, and Sharma Vimukta. "Formulation and Evaluation of Sustained Release Matrix Tablet of Nimesulide Using Pomegranate Peel and Acacia." International Journal of Pharmaceutical Sciences and Medicine 7, no. 7 (2022): 11–24. http://dx.doi.org/10.47760/ijpsm.2022.v07i07.002.

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The main objective of the study is the formulation and evaluation of sustained release matrix tablet of Nimesulide using pomegranate peel and acacia as natural polymer. The preformulation study of Nimesulide was conducted and λmax was found at 300 nm. The sustained release matrix tablet was prepared using Pomegranate peel as Release rate retardant, Acacia as polymer, Polyvinylpyrrolidone K30 as Binder, Isopropyl alcohol as Granulation solution, Micro Crystalline Cellulose as Diluent, Magnesium stearate as Lubricant and Talc as Glidant. Several formulations were prepared by taking different drug concentration in Pomegranate peel (Release rate retardant) with varying ratio of binder to lubricants. Various formulations of sustained release matrix tablet of Nimesulide F1, F2, F3, F4, F5, F6 was prepared. The prepared granules were evaluated for different parameters like Bulk density, Tapped density, Angle of repose, Carr’s index, Hausner’s ratio which shows the excellent flow properties of formulation. The physical characteristic of Nimesulide sustained release matrix tablets (F1 to F6) such as thickness, diameter, hardness, friability, weight variation and drug content were determined and results of the formulations (F1 to F6) found to be within the limits specified in official books. The drug content of all the formulation were found to be in the range of 99.59 to 99.83 % w/w, which is within the specified limit as per Indian Pharmacopoeia 1996 (i.e. 90-110% w/w). The drug released from formulation F1 to F3 was found to be 93.7, 92.9 and 92.2 % for Nimesulide respectively. The drug released from formulation F4 to F6 was found to be 94.1, 93.9 and 92.8% for Nimesulide respectively. The release rate of F1 and F4 was found to be higher when compared to other formulations this is due to increase in the concentration of polymer. These results are indicating that has higher drug retarding ability for long duration. All the formulations were analyzed for stability testing. All the formulations from F1 to F6 were found to be stable.
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Kalyani Shelar, Gauri Mahajan, Nikita Pagare, Prachiti Sahane, and Sakshi Bhosale. "Review on Sustained Release Tablet." International Journal of Scientific Research in Science and Technology 11, no. 6 (2024): 698–708. https://doi.org/10.32628/ijsrst241161126.

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This review highlights the advantages of SR formulations, including reduced side effects, enhanced drug utilization, improved treatment efficacy, and better patient compliance. Key considerations for developing sustained release tablet involve the drug's physicochemical properties and biological factors, such as absorption and metabolism. Various formulation strategies, including diffusion-controlled, dissolution-controlled, and osmotic systems, are discussed alongside essential evaluation parameters like density, hardness, and in-vitro drug release profiles. The outlook for sustained release tablets is bright , as their growing use in the pharmaceutical industry focuses on enhancing therapeutic effectiveness. Overall, sustained release tablet formulations represent a significant advancement in modern pharmacotherapy, enhancing efficacy and patient adherence to treatment regimens.
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R., Narayana Charyulu, Gandhi Kinjal B., Jobin Jose, Sneh Priya, and Shastry C. S. "INFLUENCE OF BIOENHANCERS ON THE RELEASE PATTERN OF NIOSOMES CONTAINING METHOTREXATE." Journal of Health and Allied Sciences NU 02, no. 02 (2012): 36–40. http://dx.doi.org/10.1055/s-0040-1703568.

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AbstractThe aim of present study was to prepare sustained release formulations of niosomes of methotrexate (MTX) alone (N1 to N10) and along withbioenhancers (NB1 to NB9) by thin film hydration technique using span 60 as surfactant,cholesterol as membrane stabilizing agent, curcumin and piperine as bioenhancers and dicetyl phosphate (DCP) as charge inducing agent. All the formulations of niosomeswere characterized on the basis of physical appearance and entrapment efficiency. The invitro releasestudies of optimized formulation of niosomes of MTX alone and along with bioenhancers were performed and compared with pure drug released. The entrapment efficiency of MTX in optimized formulation of niosomes containing MTX along with bioenhancers was found to 56.9% and entrapment efficiency of bioenhancerscurcumin and piperinewas found to be 40.30% and 69.1%respectively. In vitro drug release of optimized formulationsof niosomes of MTX without and with bioenhancers (F3) was found to be 98.89% and 60.97% at the end of 12 h respectively. Results concluded that Niosomes of MTX containing bioenhancers followed sustain release pattern.
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Deepthi, V. Phani, AMPAPURAM RAJESH PAVAN, G. Naresh Babu, and K. Sreenivasulu. "Formulation and Evaluation of Prulifloxacin Sustained Release Matrix Tablets." Journal of Drug Delivery and Therapeutics 9, no. 4 (2019): 72–81. http://dx.doi.org/10.22270/jddt.v9i4.2974.

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Prulifloxacin is a chemotherapeutic antibiotic of Fluor quinolone drug used to treat a various urinary tract infections. It has short half-life, makes the sustained release (SR) forms extremely advantageous. Sustained release tablets results in increased bioavailability. The purpose of the present study was to develop a sustain release matrix drug delivery system (SR) containing Prulifloxacin as a model drug by using various proportions of polymers such as HPMC E15, HPMC K15. The sustained release formulations of Prulifloxacin were prepared by direct compression method. Optimization of formulation was done by studying effect of drug to polymer ratio on drug release. FT-IR studies indicated absence of any interaction between Prulifloxacin, polymers (HPMC E15 and HPMC K15) and excipients. Ten formulations were prepared and Formulation F8 possesses good drug release property. The tablets were also evaluated for its hardness, friability and other In-vitro evaluation tests. All parameters complied with IP limits. Drug release was diffusion controlled and followed Zero order kinetics. Non-Fickian diffusion was the drug release mechanism for all the tablets formulated. Keywords: Sustained drug delivery system, Prulifloxacin, HPMCE15, HPMCK15
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Parashar, Tarun, Kapil Kalra, Jyoti M. Kalra, et al. "Formulation and In-vitro Evaluation of Bilayer Tablet of Olmesartan Medoxomil for Biphasic Drug Release." INTERNATIONAL JOURNAL OF PHARMACEUTICAL QUALITY ASSURANCE 14, no. 02 (2023): 388–92. http://dx.doi.org/10.25258/ijpqa.14.2.24.

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Objective: The current study aimed to optimize the bioavailability and absorption of olmesartan in the lower gastrointestinal tract by creating a bilayer tablet for biphasic drug release. Methods: Microcrystalline cellulose was combined and direct compression the requirement for an early response to address an undesirable defect or condition. In the current instance, 5 mg of olmesartan must be released immediately, and the remaining 10 mg of olmesartan must be released gradually to maintain the therapeutic concentration. In order to adjust the release pattern of the olmesartan sustained release tablet in accordance with the needs of therapy and IP guidelines. Result: The best cumulative drug release was demonstrated by formulation. All formulations for immediate release support the first-order kinetics. As a result, all three formulations were chosen for additional research. Dissolution rate for long-term release Cumulative drug release from the SR1 to SR3 formulations using HPMC K15M and gum acacia was up to 24 hours. Utilizing HPMC K15M and guar gum, the formulations SR1, SR2, and SR3 demonstrated cumulative drug releases of 72.66, 69.19, and 92.66%, respectively. The best cumulative release of the drug was demonstrated by formulations SR1, SR2, and SR3. Consequently, everyone was chosen for additional research. The cumulative drug release for the IR1-SR1, IR2-SR2, and IR3-SR3 bilayer tablet formulations was 95.24, 90.15, and 91.09%. Up to 12 hours of cumulative drug release from the formulation was observed. As a result, it was determined that IR1-SR1 was the best formulation out of all of them due to its strong correlation between the total cumulative percentage of medication releases and time, which was 95.24% up to 12 hours.
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Accha, D.M.1* Kshirsagar S.S.2. "Optimization and Evaluation of Modified Dosage form of Antihypertensive Drug." International Journal of Pharma Research and Technology 1, no. 4 (2022): 1–15. https://doi.org/10.5281/zenodo.7505191.

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The goal of the current study is to produce a modified dose form of the hypertension drug Valsartan. Without any issues, sustained release tablets were compressed, and the formulation's excipient ratio was left unchanged. We seek to develop drug delivery systems with a typical sustained release pattern in order to achieve therapeutic concentrations of the medications at the point of their maximum necessity in the body. Wet granulation technology was used in this research project to create sustained release matrix tablets employing a variety of polymers and excipients. The bulk density, compressibility index, total porosity, angle of repose, and drug content of the granules of various formulations were all assessed. All formulations' weighed amounts of granules contained a consistent amount of medication. The formulations for Valsartan sustained release fit Higuchi's model of drug release well, and batch F6 of the formulations which is based on weight variation, drug content, hardness, friability, in-vitro drug released profiles, and stability studies was the best of all the batches. Although F6 had a decent release rate during the research, the release occurred earlier than planned. It was discovered that formulation F6's in-vitro drug release was 94.74 2.11 for up to 24 hours. This leads us to the conclusion that, as compared to the current systems for the treatment of disease, modified dose forms of antihypertensive agents will offer considerable advantages.
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Shaheen, Shama*¹ Eisha Ganju² Rajni Dubey³ Bhaskar Kumar Gupta⁴. "Formulation and Characterization of Sustained-Release Microspheres of Oxazepam." International Journal of Pharmaceutical Sciences 3, no. 4 (2025): 1480–87. https://doi.org/10.5281/zenodo.15202138.

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The aim of this study was to formulate and characterize oxazepam-loaded microspheres for sustained drug release to enhance its therapeutic efficacy in the treatment of anxiety and insomnia. Various formulations of microspheres were prepared using HPMC, ethyl cellulose (EC), and guar gum as polymers, and their physical properties, such as yield, drug entrapment efficiency, buoyancy, and floating lag time, were evaluated. The optimized formulation (F4) exhibited a high percentage yield (73.32±0.22%) and drug entrapment efficiency (72.23±0.32%). Furthermore, F4 showed the shortest floating lag time (55±3 sec.) and the highest percentage buoyancy (76±2%), indicating its ability to remain buoyant in the gastric medium for prolonged periods. In-vitro drug release studies demonstrated that formulation F4 provided a sustained release of oxazepam over 12 hours, with 98.78% drug release, significantly improving upon the rapid release observed with marketed formulations. The release kinetics followed a zero-order release model (R² = 0.9748), ensuring a constant drug release rate. These results suggest that oxazepam-loaded microspheres could serve as an effective sustained-release formulation for long-term management of anxiety disorders, reducing dosing frequency and improving patient compliance.
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Dissertations / Theses on the topic "Sustained Release Formulations"

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Purkiss, Ronald. "Bioequivalence of sustained release theophylline formulations." Thesis, Aston University, 1986. http://publications.aston.ac.uk/12472/.

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The bioequivalence of sustained release theophylline formulations, marketed in the United Kingdom, has been investigated in relation to the co-administration of food in both single dose and steady state volunteer studies. The effect of food on pharmacokinetic parameters and their clinical relevance was researched. Experimentation using drug induced modification of gastric motility to ascertain the component influences of the rate of gastric emptying on the absorption of theophylline from sustained release formulations was conducted. Prolongation of time to maximum plasma theophylline concentration by food reported in the literature and its clinical importance was investigated in once daily compared with twice daily administration of sustained release theophylline formulations and smoking habit. The correlation between saliva and plasma theophylline concentrations as a means of developing a non-invasive sampling techniques was examined. Data obtained from in vitro dissolution studies was compared with in vivo results. This thesis has shown no significant differences occurred in the pharmacokinetic parameters measured between sustained release formulations available in the United Kingdom. The investigations into the influence of food on prolongation of time to maximum plasma theophylline concentration and other measured pharmacokinetic parameters demonstrated no important pharmacokinetic or clinical effects. Smoking adults taking sustained release theophylline formulations had similar drug clearances to those reported in the literature for smokers taking plain uncoated theophylline formulations.
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Lee, Jobina J. N. "Investigations into sustained-release hydrophobic matrix pellet formulations." Thesis, University of Strathclyde, 2003. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.275167.

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Wagner, Daniel. "Sustained release formulations for compounds underlying intestinal drug efflux." [S.l.] : [s.n.], 2003. http://deposit.ddb.de/cgi-bin/dokserv?idn=96927890X.

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Sachikonye, Tinotenda Chipo Victoria. "Development and assessment of minocycline sustained release capsule formulations." Thesis, Rhodes University, 2010. http://hdl.handle.net/10962/d1013127.

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The use of minocycline for the treatment of a broad range of systemic infections and for severe acne has been associated with vestibular side effects. The severity of side effects may lead to poor adherence to therapy by patients. The use of sustained release formulations of minocycline that display slow dissolution of minocycline following administration may be beneficial in reducing the incidence and severity of side effects. Therefore, sustained release capsule dosage forms containing 100 mg minocycline (base) were manufactured and assessed for use as sustained release oral dosage forms of minocycline. Minocycline sustained release capsules were manufactured based on matrix technologies using hydroxypropylmethyl cellulose (HPMC) and Compritol® as release retarding polymers. The rate and extent of minocycline release from the capsules was evaluated using USP Apparatus 1 and samples were analysed using a validated High Performance Liquid Chromatographic (HPLC) method with ultraviolet (UV) detection. Differences in the rate and extent of minocycline release from formulations manufactured using HPMC or Compritol® were influenced by the concentration of polymer used in the formulations. The rate and extent of minocycline release was faster and greater when low concentrations of polymer were used in formulations. The effect of different excipients on the release pattern(s) of minocycline and particularly their potential to optimise minocycline release from experimental formulations was investigated. The use of diluents such as lactose and microcrystalline cellulose (MCC) revealed that lactose facilitated minocycline release when HPMC was used as the polymer matrix. In contrast, the use of lactose as diluent resulted in slower release of minocycline from Compritol® based formulations. The addition of sodium starch glycolate to HPMC based formulations resulted in slower release of minocycline than when no sodium starch glycolate was used. Compritol® based formulations were observed to release minocycline faster following addition of sodium starch glycolate and Poloxamer 188 to experimental formulations. In vitro dissolution profiles were compared to a target or reference profile using the difference and similarity factors, ƒ1 and ƒ2 , and a one way analysis of variance (ANOVA). In addition, the mechanism of minocycline release was elucidated following fitting of dissolution data to the Korsmeyer-Peppas, Higuchi and Zero order models. Minocycline release kinetics were best described by the Korsmeyer-Peppas model and the values of the release exponent, n (italics), revealed that drug release was a result of the combined effects of minocycline diffusion through matrices and erosion of the matrices. These in vitro dissolution profiles were better fit to the Higuchi model than to the Zero order model. Two formulations that displayed a fit to the Zero order model were identified for further studies as potential dosage forms for sustained release minocycline.
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Janoria, Kumar Gaurav Mitra Ashim K. "Transporter targeted prodrug approach and sustained release formulations for ocular delivery of ganciclovir." Diss., UMK access, 2008.

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Thesis (Ph. D.)--School of Pharmacy and Dept. of Chemistry. University of Missouri--Kansas City, 2008.<br>"A dissertation in pharmaceutical sciences and chemistry." Advisor: Ashim K. Mitra. Typescript. Vita. Description based on contents viewed Sept. 12, 2008; title from "catalog record" of the print edition. Includes bibliographical references (leaves 193-204). Online version of the print edition.
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Hildebrandt, Christian. "Crystalline Monoclonal Antibodies: Development of stable crystals for drying and sustained release formulations." Diss., Ludwig-Maximilians-Universität München, 2014. http://nbn-resolving.de/urn:nbn:de:bvb:19-174392.

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Marquette, Sarah. "Stabilization and development of sustained-release formulations of protein/antibody for subcutaneous delivery." Doctoral thesis, Universite Libre de Bruxelles, 2014. http://hdl.handle.net/2013/ULB-DIPOT:oai:dipot.ulb.ac.be:2013/209251.

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ABSTRACT<p><p>This project aimed at developing a drug delivery system (DDS) able to enhance the stability and<p>residence time in vivo of antibodies (Abs). The system will deliver drug by the subcutaneous<p>route (SC), while ensuring accurate control of the drug release and the resulting plasmatic level. This technology platform will allow to reduce frequency of injection, potentially decrease side effects and maintain high concentration of Abs which will improve life of patient having chronic disease such as autoimmune and inflammatory disease. Biodegradable synthetic polymer-based formulations (polylactide-co-glycolide (PLGA)) were selected as carriers for encapsulated Abs. This was because they offer good protection for the Abs and allow sustained release of the Abs for a controlled period of time. After the evaluation of different encapsulation methods such as the water-oil-in-water (w/o/w) and the solid-in-oil-inwater<p>(s/o/w) processes, the encapsulation of the Ab in solid state (s/o/w) appeared to be more appropriate for producing Ab-loaded PLGA microspheres (MS). It allowed us to maintain the<p>Ab in a monomeric conformation and to avoid the formation of unsoluble aggregates mainly present at the water/oil interface. The first part of the project was the optimization of both the method for producing the Ab solid particles (spray-drying process) and the encapsulation of these Ab solid particles into the polymeric MS (s/o/w process) by design of experiment (DoE). These optimizations were carried out using a bovine polyclonal immunoglobulin G (IgG) as model molecule. In further optimization of the spray-drying process by (DoE), aqueous Ab solutions were spray-dried using a mini Spray-Dryer assembly with a 0.7 mm spray nozzle. In accordance with the particle size (d(0.5) ~5 μm), the stability (no loss of monomer measured by<p>size exclusion chromatography (SEC) and the yield of the spray-drying process (> 60 % w/w), the process parameters were set of follow: 3 mL/min as liquid feed flow rate, 130°C /75°C as inlet temperature (inlet T°) / outlet temperature (outlet T°), 800 L/h as atomization flow rate and<p>30 m3/h as drying air flow rate. For the s/o/w, the methylene chloride (MC) commonly used for<p>an encapsulation process was replaced by ethyl acetate (EtAc), which was considered as a more<p>suitable organic solvent in terms of both environmental and human safety. The effects of several processes and formulation factors were evaluated on IgG:PLGA MS properties such as: particle size distribution, drug loading, IgG stability, and encapsulation efficiency (EE%). Several formulations and processing parameters were also statistically identified as critical to get reproducible process (e.g. the PLGA concentration, the volume of the external phase, the emulsification rate, and the quantity of IgG microparticles). The optimized encapsulation<p>method of the IgG has shown a drug loading of up to 6 % (w/w) and an encapsulation efficiency<p>of up to 60 % (w/w) while preserving the integrity of the encapsulated antibody. The produced MS were characterized by a d(0.9) lower than 110 μm and showed burst effect lower than 50 %(w/w). In the second part of the project, the optimized spray-drying and s/o/w processes<p>developed with the IgG were applied to a humanized anti-tumor necrosis factor (TNF) alpha<p>MAb to confirm the preservation of the MAb activity during these processes. The selected s/o/w method allowed us to produce MAb-loaded PLGA MS with an appropriate release profile up to 6 weeks and MAb stability. In order to maintain the Abs’ activity, both during encapsulation and<p>dissolution, the addition of a stabilizer such as trehalose appeared to be crucial, as did the<p>selection of the PLGA. It was demonstrated that the use of a PLGA characterized by a 75:25<p>lactide:glycolide (e.g. Resomer ® RG755S) ratio decreased the formation of low molecular weight species during dissolution, which led to preserve Abs activity through its release from the<p>delivery system. Furthermore, the release profile was adjusted according to the type of polymer<p>and its concentration. E.g. 10 % w/v RG755S allowed Ab MS with a release time of 6 weeks to<p>be obtained. The optimization of both the formulation and the encapsulation process allowed<p>maximum 13 % w/w Ab-loaded MS to be produced. It was demonstrated that the Ab-loaded PLGA MS were stable when stored at 5°C for up to 12 weeks and that the selection of the appropriate type of PLGA was critical to assuring the stability of the system. The better stability observed when using a PLGA characterized by a 75:25 lactide:glycolide ratio was attributed to<p>its slower degradation rate. Finally, the sustained release of Ab from the developed MS and the preservation of its activity was confirmed in vivo in a pharmacokinetic (pK) study realized in<p>rats. In conclusion, the application of the concept of entrapment into a polymer matrix for<p>stabilization and sustained release of biological compounds was demonstrated through this work.<p><p><p><p>RÉSUMÉ<p><p>Ce projet a pour but de développer un système de délivrance de médicament capable d’augmenter la stabilité et le temps de résidence in vivo des anticorps. Ce système sera administré par voie sous-cutanée et permettra un control précis de la libération du produit et de son niveau plasmatique. Cette plateforme technologique nous permettra de réduire la fréquence d’injection, de réduire potentiellement les effets secondaires et de maintenir des concentrations élevées en anticorps tout en améliorant la vie des patients atteints de maladies chroniques autoimmunes ou inflammatoires. Les formulations à base de polymères synthétiques, biodégradables (PLGA) ont été sélectionnés comme véhicules pour encapsuler les anticorps. Ils offrent en effet une bonne protection pour les anticorps and permettent une libération contrôlée de ceux-ci pendant une période définie. Après l’évaluation de différents méthodes d’encapsulation tels que les procédés d’eau-dans-huile-dans-eau (w/o/w) et solide-dans-huile-dans-eau (s/o/w), l’encapsulation des anticorps sous forme solide apparaissait plus apporpriée pour produire des microsphères de polymère chargées en anticorps. Cette technique nous permettait de maintenir l’anticorps sous sa forme monomérique et d’éviter la formation d’agrégats insolubles qui apparaissaient principalement à l’interface eau/huile. La première partie du projet a été d’optimiser à la fois la méthode nous permettant d’obtenir les anticorps sous forme de particules solides (spray-drying) et la méthode d’encapsulation de ces particules d’anticorps dans les microsphères de polymères. Cela a été réalisé par des plans d’expérience en utilisant une IgG bovine polyclonale comme molécule modèle. Durant l’optimisation du procédé de spray-drying,<p>les solutions aqueuses d’anticorps ont été atomisées en utilisant le mini Spray-Dryer assemblé avec une buse de pulvérisation d’un diamètre de 0.7 mm. En accord avec la taille particulaire (d(0.5) ~5 μm), la stabilité (absence de perte en monomère mesurée par chromatographie d’exclusion de taille et le rendement d’atomisation (> 60 % w/w), les paramètres d’atomisation ont été fixés: 3 mL/min pour le débit de liquide, 130°C /75°C pour la température d’entrée / température de sortie, 800 L/h pour le débit d’air d’atomisation et 30 m3/h pour le débit d’air de séchage. Pour le s/o/w, le dichlorométhane communément utilisé dans les procédés d’encapsulation a été remplacé par l’acétate d’éthyle qui est considéré comme un meilleure solvant organique en terme d’environnement et de sécurité. Les effets de plusieurs paramètres de fabrication ou de formulation ont été évalués sur les propriétés des microsphères polymériques d’anticorps (distribution de taille particulaire, taux de charge en anticorps, stabilité de l’anticorps et efficacité d’encapsulation). Plusieurs paramètres de fabrication et de formulation ont été statistiquement identifiés comme critiques pour obtenir un procédé reproductible (par exemple. La concentration en PLGA, le volume de phase externe, la vitesse d’émulsification et la quantité d’anticorps). La méthode d’encapsulation ainsi optimisée permettait d’obtenir un taux<p>de charge jusqu’à 6% (w/w) avec une efficacité d’encapsulation jusqu’à 60 % (w/w) tout en<p>préservant l’intégrité de l’anticorps encapsulé. Les microsphères produites étaient caractérisées<p>par un d(0.9) inférieur à 110 μm et montraient une libération après 24 h inférieure à 50 % (w/w).<p>Dans le seconde partie du projet, les procédés d’atomisation et d’encapsulation développés avec<p>l’IgG ont été appliqués à un anticorps monoclonal anti-TNF alpha humanisé pour confirmer la<p>conservation de l’activité de l’anticorps pendant ces procédés. La méthode s/o/w sélectionnée<p>permettait de produire des microsphères de PLGA chargées en anticorps avec un profil de libération jusqu’à 6 semaines et un maintien de la stabilité de l’actif. Afin de maintenir l’activité de l’anticorps, à la fois pendant le procédé d’encapsulation et pendant la libération, l’ajout d’un stabilisant tel que le tréhalose est apparu crucial ainsi que le choix du type de PLGA. Il a été démontré que l’utilisation du PLGA caractérisé par un ratio lactide :glycolide de 75 :25 (par exemple, Resomer ® RG755S) diminuait la formation d’espèces de faible poids moléculaire<p>pendant la dissolution. Cela contribuait à préserver l’activité de l’anticorps durant la libération à partir des microsphères. De plus, le profil de libération était modulé en fonction du type de polymère et de sa concentration. Par exemple, l’utilisation d’une solution à 10 % w/v RG755S conduisait à la production de microsphères d’anticorps avec un temps de libération sur 6<p>semaines. L’optimisation de la formulation et du procédé d’encapsulation a permis de produire<p>des microsphères avec des taux de charge en anticorps de maximum 13 % w/w. Il a été démontré<p>que ces microsphères, stockées à 5°C, étaient stables jusqu’à 12 semaines et que la sélection du<p>type de PLGA était critique pour assurer la stabilité du système. La meilleure stabilité a été<p>obtenue en utilisant le PLGA caractérisé par un ratio lactide :glycolide de 75 :25. Cela a été<p>attribué à sa plus faible vitesse de dégradation. Enfin, la libération contrôlée de l’anticorps à<p>partir de ces microsphères et la conservation de son activité ont été confirmées in vivo lors d’une<p>étude pharmacocinétique réalisée chez le rat. En conclusion, ce travail a permis de démontrer<p>l’application du concept d’ « emprisonnement » des composés biologiques dans des matrices<p>polymériques afin de les stabiliser et contrôler leur libération.<br>Doctorat en Sciences biomédicales et pharmaceutiques<br>info:eu-repo/semantics/nonPublished
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Ruberg, Eva-Maria. "Development of sustained release formulations for the intra-articular delivery of a therapeutic antibody." Diss., Ludwig-Maximilians-Universität München, 2013. http://nbn-resolving.de/urn:nbn:de:bvb:19-183255.

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Hildebrandt, Christian [Verfasser], and Gerhard [Akademischer Betreuer] Winter. "Crystalline Monoclonal Antibodies: Development of stable crystals for drying and sustained release formulations / Christian Hildebrandt. Betreuer: Gerhard Winter." München : Universitätsbibliothek der Ludwig-Maximilians-Universität, 2014. http://d-nb.info/1059351412/34.

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Nieto, Bobadilla Maria Susana. "A new antibacterial agent : in vitro bacteriological characterization and in vitro/in vivo performance of sustained release formulations." Thesis, Lille 2, 2015. http://www.theses.fr/2015LIL2S018/document.

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Introduction : La résistance aux antibiotiques est une menace de santé, il est donc urgent de développer de nouveaux antibactériens. CIN-102, est un nouvel antibactérien développé par une industrie pharmaceutique. Il possède un large-spectre d’action et aucune résistance n’a été développée jusqu’à présent. Parmi les possibles applications thérapeutiques du CIN-102, notre recherche s’est focalisée sur les Maladies Inflammatoires Chroniques de l’Intestin (MICIs). Plusieurs facteurs contribuent à l’étiologie des MICIs. Les bactéries intestinales jouent un rôle important dans ces maladies et une augmentation de la charge bactérienne est observée pendant l’inflammation. Les objectifs de ce travail ont été : la caractérisation de l’activité antibactérienne du CIN-102, l’analyse de l’activité antibactérienne des agents anti-inflammatoires et antibiotiques utilisés en cas de MICI et la fabrication des formulations à ciblage colique pour le CIN-102. Le but est de diminuer la charge bactérienne colique par moyen du CIN-102 et améliorer, de cette façon, l’état de l’inflammation.Méthodes: La Concentration Minimale Inhibitrice (CMI), l’Effet Post-Antibiotique (EPA) et le temps de réduction logarithmique du CIN-102 ont été déterminés pour des bactéries aérobies et anaérobies. Les interactions entre le CIN-102 et des antibiotiques sur le marché ont été évaluées. La CMI de l’acide 5-aminosalicylique (5-ASA), GED-0507-34 et antibiotiques ont été déterminées pour des souches anaérobiques. Par rapport aux formulations à libération prolongée : des mini-granules contenant le CIN-102 ont été fabriqués par extrusion-sphéronisation puis pelliculés avec des mélanges de polymères insolubles et polysaccharides. Parallèlement, des mini-comprimés de CIN-102 ont été fabriqués par compression directe. La libération du CIN-102 in vitro, a été mesurée dans des milieux simulant l’estomac et l’intestin grêle. L’efficacité des systèmes à libération prolongée a été évaluée dans un modèle de colite chez la souris. Des prélèvements de selles et tissus coliques ont été soumis à des études bactériologiques. L’expression des cytokines a été mesurée à partir des tissus coliques.Résultats et discussion : Le large-spectre d’action du CIN-102 a été confirmé. Toutes les souches ont été inhibées par le CIN-102. CIN-102 présente un EPA et un temps de réduction logarithmique court. Il présente des interactions synergiques avec plusieurs antibiotiques, notamment la colistine et les aminoglycosides, en les rendant actifs contre des bactéries multirésistantes. Ces résultats in vitro doivent être poursuivis par des études chez l’animal. Des agents anti-inflammatoires utilisés contre les MICIs ne possèdent pas d’activité antibactérienne. Par ailleurs, les antibiotiques testés n’ont pas un large-spectre d’action contre des bactéries anaérobies généralement retrouvées dans l’intestin. Cela confirme le besoin d’un antibiotique à large spectre capable de réduire des charges bactériennes en cas d’inflammation. Dans ce but, des formulations capables de délivrer CIN-102 au niveau du colon ont été étudiées. La libération du CIN-102 des mini-granules pelliculés et mini-comprimés a été réduite dans des milieux simulant l’estomac et l’intestin grêle. Des souris atteintes de colite et traitées avec les formulations du CIN-102 ont eu une diminution des diarrhées et du sang dans les selles. Les concentrations d’entérobactéries adhérentes à la muqueuse colique et dans les selles ont été significativement réduites chez les souris traitées avec le CIN-102. Ces résultats montrent que ces formulations peuvent délivrer CIN-102 dans le tractus gastro-intestinal inferieur, et que la diminution d’entérobactéries semble réduire les symptômes de la colite.Conclusion : CIN-102 est un nouvel antibactérien a large-spectre et des formulations à libération prolongée peuvent délivrer cet agent dans le colon, diminuant la charge d’entérobactéries qui pourrait influencer l’état de l’inflammation<br>Introduction: Antibiotic resistance is a major threat to public health and new antimicrobials are urgently needed. CIN-102, a new antibacterial agent which resembles cinnamon essential oils composition, was developed by a pharmaceutical company. CIN-102 had a broad-spectrum of action and resistance was not developed until now. Between all the possible therapeutic applications for CIN-102, a future utilization against Inflammatory Bowel Diseases (IBD) is aimed. IBD are chronic pathologies with a multifactorial etiology. In this context, enteric bacteria are well-known to have an important role, and higher bacterial concentrations are found in the intestine under inflammatory conditions. The objectives of this work were: to characterize the bacteriological activity of CIN-102, to analyze the bacteriological activity of anti-inflammatory agents and antibiotics used in IBD and to fabricate multiparticulate CIN-102 pharmaceutical forms for colonic targeted drug release. The idea is to use CIN-102 to reduce colonic bacterial loads and improve the state of intestinal inflammation. Methodology: The Minimal Inhibitory Concentration (MIC), the Post-Antibiotic Effect (PAE) and the logarithmic reduction time of CIN-102 were determined against several aerobic and anaerobic bacterial isolates. The interactions between CIN-102 and commercialized antibiotics were evaluated. The MIC of 5-aminosalicilyc acid, GED-0507-34 and antibiotics were determined for anaerobic bacterial isolates. Concerning sustained released formulations: CIN-102 pellet cores were fabricated by extrusion-spheronization and subsequently coated with blends of insoluble polymers and natural biodegradable polysaccharides. CIN-102 mini-tablets were fabricated by direct compression. In vitro drug released was measured in simulated gastric and intestinal fluid. The efficacy of best sustained release formulations was assessed in a murine model of colitis. Samples of luminal contents and sections of the colon were taken to perform a bacteriological analysis. Expression of cytokines was analyzed from colonic tissues.Results and discussion: The broad-spectrum activity of CIN-102 was confirmed. All aerobic and anaerobic strains were susceptible to CIN-102. Furthermore, CIN-102 had an important PAE and exerted a fast logarithmic reduction of bacterial inoculum. It interacts synergistically with several antibiotics, mostly with colistin and aminoglycosides, restoring the antibiotic activity against multi-resistant bacteria. The promising in vitro activity of CIN-102 has to be further confirmed by animal studies. Anti-inflammatory agents used against IBD were not provided of antibacterial activity and neither of the antibiotics tested possessed a broad-spectrum of action against anaerobic isolates commonly found in the intestine. These results confirm the need of a broad-spectrum antibiotic capable of reduced increased bacterial loads during inflammation. Following this aim, oral dosage forms able to deliver CIN-102 into the colon were studied. Concerning the sustained release forms, in vitro CIN-102 release from coated-pellets and mini-tablets was reduced in simulated gastric and intestinal fluids. Colitic mice treated with CIN-102 controlled release formulations had less diarrhea and bloody stools. Furthermore, the concentrations of enterobacteria in colonic tissue and stool were significantly reduced in CIN-102 treated mice. These results show that sustained release formulations can effectively deliver CIN-102 in the lower part of the gastrointestinal tract, where the reduction of enterobacteria seems to ameliorate the course of colitis.Conclusion: CIN-102 is novel broad-spectrum antibacterial and sustained release formulations can effectively deliver this agent into the colon, reducing bacterial loads which might influence the state of intestinal inflammation
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Books on the topic "Sustained Release Formulations"

1

Purkiss, Ronald. Bioequivalence of sustained release theophylline formulations. Aston University. Department of Pharmaceutical Sciences, 1986.

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Avraham, Yacobi, Halperin-Walega Eva, and American Pharmaceutical Association, eds. Oral sustained release formulations: Design and evaluation. Pergamon Press, 1988.

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Yacobi, Avraham. Oral Sustained Release Formulations: Design and Evaluation. Pergamon Pr, 1988.

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Yacobi, Avraham. Oral Sustained Release Formulations: Design and Evaluation. Pergamon Pr, 1988.

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Chou, Joyce Tian-wei. Product formulations and in vitro-in vivo evaluation of 1) topical insect repellent formualtions against mosquitoes; 2) oral sustained release formulations of cefaclor and pentoxifylline in adults. 1995.

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Sorasuchart, Waranush. (1): Evaluation of polycarbophil coated liposomes and membrane permeation of free and liposomal drugs; (2) : in vitro-in vivo evaluation of nicardipine HCl sustained-release formulations. 1998.

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Bhadra, Subrata. Nitroglycerin Sustained Release Tablet. Formulation Design and Evaluation. GRIN Verlag GmbH, 2013.

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Acri, Jane B., and Phil Skolnick. Novel Approaches for Treating Addiction. Edited by Dennis S. Charney, Eric J. Nestler, Pamela Sklar, and Joseph D. Buxbaum. Oxford University Press, 2017. http://dx.doi.org/10.1093/med/9780190681425.003.0048.

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Despite remarkable progress in our understanding of the neurobiological bases of drug abuse, no novel pharmacotherapies have recently been approved to treat substance use disorders (SUDs). Thus, while reformulations of established treatments have either been approved or are currently in late stage development (e.g., sustained release formulations of naltrexone (Vivitrol®) and buprenorphine), the development of medications to treat SUDs has lagged well behind other areas of psychiatry. In this chapter, we review some of the factors that have contributed to this dearth of innovative pharmacotherapies. We also review evidence that supports clinical testing of late stage molecules (developed for other indications) acting at promising targets, as well as novel biological approaches to the treatment of SUDs.
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Farrar, Keith Thomas. A comparison of the relative bioavailability and release profiles of standard and sustained-release formulationsof indomethacin. 1985.

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Awosika, Ajoritsedere. Biopharmacy of sustained-release theophylline: Design criteria for sustained-release (SR) medicines and analysis of performance of U.K.-licenced theophylline products : formulation of a new SR granular product with improved in vitro and in vivo characteristics. 1985.

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Book chapters on the topic "Sustained Release Formulations"

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Patel, Kavil, and Fang Liu. "Advanced Oral Sustained-Release Drug Delivery Systems for Older Patients." In Pharmaceutical Formulations for Older Patients. Springer International Publishing, 2023. http://dx.doi.org/10.1007/978-3-031-35811-1_6.

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Gerlach, M., B. Gebhardt, W. Kuhn, and H. Przuntek. "Pharmacokinetic studies with sustained-release formulations of levodopa in healthy volunteers." In Continuous Dopaminergic Stimulation in Parkinson’s Disease. Springer Vienna, 1988. http://dx.doi.org/10.1007/978-3-7091-8954-2_18.

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Sheokand, Mansi, Karuna Jain, Vineeta Rana, et al. "Nanobiochar-Based Formulations for Sustained Release of Agrochemicals in Precision Agriculture Practices." In Handbook of Green and Sustainable Nanotechnology. Springer International Publishing, 2023. http://dx.doi.org/10.1007/978-3-031-16101-8_109.

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Sheokand, Mansi, Karuna Jain, Vineeta Rana, et al. "Nanobiochar-Based Formulations for Sustained Release of Agrochemicals in Precision Agriculture Practices." In Handbook of Green and Sustainable Nanotechnology. Springer International Publishing, 2023. http://dx.doi.org/10.1007/978-3-030-69023-6_109-1.

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Richard, J., F. Deschamps, A. M. De Conti, and O. Thomas. "Using a Supercritical Fluid-Based Process: Application to Injectable Sustained-Release Formulations of Biomolecules." In ACS Symposium Series. American Chemical Society, 2006. http://dx.doi.org/10.1021/bk-2006-0924.ch016.

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Badaoui, Fatima Zohra, Souha Meziani, Lina Benmegoura, and Souha Djoumana Hedna. "Formulation and Optimization of Sustained Release Microparticles of Ketoprofen." In Springer Proceedings in Materials. Springer Nature Singapore, 2024. http://dx.doi.org/10.1007/978-981-97-1916-7_6.

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Akhras, F., J. Chambers, and G. Jackson. "An Interim Report on the Efficacy of Isosorbide-5-Mononitrate in a Sustained Release Formulation in Patients with Stable Angina." In Mononitrate II. Springer Berlin Heidelberg, 1987. http://dx.doi.org/10.1007/978-3-642-72689-7_23.

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Sankaram, Mantripragada. "Commercial Sustained-Release Injectable Formulations by Encapsulation." In Sustained-Release Injectable Products. CRC Press, 2000. http://dx.doi.org/10.1201/b14421-4.

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"Product Development Principles of Sustained-Release Injectable Formulations." In Sustained-Release Injectable Products. CRC Press, 2000. http://dx.doi.org/10.1201/b14421-3.

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Murdan, Sudaxshina, and Alexander Florence. "Non-aqueous Solutions and Suspensions as Sustained-Release Injectable Formulations." In Sustained-Release Injectable Products. CRC Press, 2000. http://dx.doi.org/10.1201/b14421-6.

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Conference papers on the topic "Sustained Release Formulations"

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Eriksson, Johanna, Eric Sjögren, Jean-Yves Gillon, et al. "PA-298 Predicting disease effect on the pharmacokinetics (PK) of sustained and immediate release formulations by applying physiologically based pharmacokinetic (PBPK) modelling." In Abstracts of The Eleventh EDCTP Forum, 7–10 November 2023. BMJ Publishing Group Ltd, 2023. http://dx.doi.org/10.1136/bmjgh-2023-edc.149.

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Gupta, Rishabh, Sonia Dhiman, Chaitali Agrawal, Sonal Sharma, and Thakur Gurjeet Singh. "Formulation and evaluation of nateglinide-loaded nanostructured lipid carriers for sustained release." In THE FIFTH SCIENTIFIC CONFERENCE FOR ELECTRICAL ENGINEERING TECHNIQUES RESEARCH (EETR2024). AIP Publishing, 2024. http://dx.doi.org/10.1063/5.0228716.

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Sandri, Monica, Michele Iafisco, Silvia Panseri, Elisa Savini, and Anna Tampieri. "Fully Biodegradable Magnetic Micro-Nanoparticles: A New Platform for Tissue Regeneration and Theranostic." In ASME 2013 2nd Global Congress on NanoEngineering for Medicine and Biology. American Society of Mechanical Engineers, 2013. http://dx.doi.org/10.1115/nemb2013-93223.

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Nowadays, magnetic materials are receiving special attention due to their potential applications in different fields and in particular in medicine. Magnetic micro-nano-particles have been progressively employed as support materials for enzyme immobilization, and have been used as drug-delivery vehicles, contrast agents for magnetic resonance imaging as well as heat mediators for hyperthermia-based anti-cancer treatments and many other exciting biomedical applications. Magnetic materials have also attracted a big interest in the field of bone tissue regeneration because it has been demonstrated that magnetic nanoparticles have effect of osteoinduction even without external magnetic force. Therefore, one of the most big challenge in this field is the production of magnetic materials with good biocompatibility and biodegradability. In fact, the long-term effects in the human body of iron oxide (maghemite or magnetite), the most popular magnetic phase used in medicine and biotechnology, are not yet completely assessed. To this aim, in this work we developed an innovative biocompatible and bioresorbable superparamagnetic-like phase by doping nano-hydroxyapatite with Fe2+/Fe3+ ions (FeHA). Moreover the same magnetic nanoparticles were used as nano-particulate emulsifier for the preparation of hollow hybrid Fe-HA-poly(L-lactic) acid (PLLA) micro-nano-spheres. PLLA has been used because poly(α-hydroxy-esters) are the most frequently used synthetic polymers for biomedical applications owing to their biocompatibility, hydrolytic degradation process and proper mechanical properties. These micro-nanospheres could be used as new type of scaffold for hard tissue regeneration. In fact, spherical scaffold display several advantages respect to the monolithic counterpart e.g., (i) improving control over sustained delivery of therapeutic agents, signalling biomolecules and even pluripotent stem cells, (ii) serving as stimulus-sensitive delivery vehicles for triggered release, (iii) introducing porosity and/or improve the mechanical properties of bulk scaffolds by acting as porogen or reinforcement phase, (iv) supplying compartmentalized micro-reactors for dedicated biochemical processes, (v) functioning as cell delivery vehicle, and, finally, (vi) giving possibility of preparing injectable and/or mouldable formulations to be applied by using minimally invasive surgery. Moreover, the same magnetic materials could find applications in nanomedicine as a multifunctional carrier. Their magnetic functionality could be utilized to move them into the body towards target organs by an external magnetic field. Furthermore, the superparamagnetic feature of the nanoparticles could allow to tailor the release of the therapeutic agent by switching (on-off) the external magnetic field and/or to treat cancer cells by hyperthermia.
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Sipos, Bence, Márk Benei, Ildikó Csóka, and Gábor Katona. "Formulation of sustained release sodium alginate beads loaded with antidiabetic drug containing polymeric micelles." In V. Symposium of Young Researchers on Pharmaceutical Technology,Biotechnology and Regulatory Science. Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Faculty of Pharmacy, 2023. http://dx.doi.org/10.14232/syrptbrs.2023.51.

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Wu, Tzung-Ju, Wan-Ni Yu, Ming-Ju Wu, Po-Chun Chang, and Sheue-Fang Shih. "THU0465 PHARMACOKINETICS AND TOXICOKINETICS STUDIES OF A SUSTAINED RELEASE LIPOSOMAL FORMULATION OF DEXAMETHASONE SODIUM PHOSPHATE (TLC599) FOLLOWING INTRA-ARTICULAR INJECTION IN DOGS." In Annual European Congress of Rheumatology, EULAR 2019, Madrid, 12–15 June 2019. BMJ Publishing Group Ltd and European League Against Rheumatism, 2019. http://dx.doi.org/10.1136/annrheumdis-2019-eular.3880.

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Stow, Simon R., and Ann P. Dowling. "Modelling of Circumferential Modal Coupling Due to Helmholtz Resonators." In ASME Turbo Expo 2003, collocated with the 2003 International Joint Power Generation Conference. ASMEDC, 2003. http://dx.doi.org/10.1115/gt2003-38168.

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Lean premixed prevaporised (LPP) combustion can reduce NOx emissions from gas turbines, but often leads to combustion instability. Acoustic waves produce fluctuations in heat release, for instance by perturbing the fuel-air ratio or flame shape. These heat fluctuations will in turn generate more acoustic waves and in some situations self-sustained oscillations can result. A linear model for thermoacoustic oscillations in LPP combustors is described. A thin annular geometry is assumed and so circumferential modes are included but radial dependence is ignored. The formulation is in terms of a network of modules such as straight ducts and area changes. At certain operating conditions, the flow is predicted to be unstable, with linear waves growing in amplitude. Helmholtz resonators can be used to absorb acoustic energy and, when carefully designed and installed at appropriate locations, can stabilise the flow. Helmholtz resonators are included in the model. Connecting a Helmholtz resonator to an annular duct destroys the axisymmetry of the geometry. This results in coupling of the circumferential modes which must be calculated. The model is used to investigate the best arrangement of resonators around the circumference of an annular duct to achieve maximum damping of a circumferential oscillation.
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Reports on the topic "Sustained Release Formulations"

1

Chutimaworapan, Suchada, Chaiyo Chaichantippayuth, and Areerat Laopaksa. Formulation of pharmaceutical products of Garcinia mangostana Linn. extracts. Chulalongkorn University, 2006. https://doi.org/10.58837/chula.res.2006.32.

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Part I: The purpose of the investigation was to develop the extraction process that was simple, practical and giving high yield. The maceration of dried powder of Garcinia mangostana fruit husk with ethyl acetate gave yellow crystalline powder of mangostin. The yield was calculated as 7.47%. The identification of the Garcinia mangostanahusk extract was carried out by thin-layer chromatography (TLC) and differential scanning calorimetry. The TLC of mangostin was done by using the alumina sheet and ethyl acetate: hexane (3:1) as mobile phase. The Rf value as compared with standard mangostin was 0.60. The DSC thermogram showed the board melting range of the crude extract at 165.04-166.80 °C. The quantitative analyses of mangostin were developed using the high performance liquid chromatography (HPLC) and ultraviolet (UV) spectrophotometry. The HPLC system using methanol: water (87:13) as mobile phase, clotrimazole as internal standard and using UV detector at 243 nm. The UV spectrophotometric method was carried out using the UV spectrophotometer at 243 nm. The validation of both systems gave high specificity, linearity, accuracy and precision. The solubility study of mangostin showed the low water insolubility. The water solubility was improving with increasing ethanol content. The in vitro microbiological activity of mangostin to Staphylococcus aureus ATCC 25923 and Streptococcus mutans ATCC KPSK2 was studied. The minimum inhibitory concentrations of the extract were 3 µg/ml and 1.5 µg/ml, respectively. The minimum bactericidal concentrations of the extract was 4 µg/ml and 3 µg/ml, respectively.Part II: The purpose of this study was to develop fast dissolving oral strips containing Garcinia mangostana husk extract. The films consisted of low viscosity hydrophilic polymers such as hydroxypropyl methylcellulose and hydroxypropylcellulose, acesulfame potassium as sweetener, and menthol and eucalyptus oil as flavoring agents. The physical and mechanical properties and dissolution time of film bases were compared with commercial product strips A. From the dissolution time data, it was found that the film prepared from mixed polymer between HPMC 3 cps and HPC LV at ratios 2:1, 3:1, 4:1 and 5:1 were not significantly different from commercial product strips A (p&gt;0.05). The films containing extract were light yellow and had porous surface based on observation from scanning electron microscopy. The dissolution profiles of all formulations showed the rapid release more than 80 percent of mangostin from films within 3-7 minutes and the fastest release was from formulation of HPMC 3 cps and HPC LV at ratio 5:1. Differential scanning calorimetry results exhibited that the Garcinia mangostana extract and additives were not in crystalline form in the films. The fast dissolving oral strips containing Garcinia mangostana husk extract showed in vitro antimicrobial activity against oro-dental bacteria, namely, Staphylococcus aureus aTCC 25923 and Streptococcus mutans ATCC KPSK2. Unter strese conditions at 40 degree Celcius and 75 percent relative humidity, the strips showed a good stability.The purpose of the study was to develop monoglyceride-based drug delivery systems containing Garcinia Mangostana extract. The system is based on the ability of mixtures of monoglyceride (dlyceryl monooleate) and triglycerides to form liquid crystals upon contact with water. The drug delivery systems can be administered by syringe and transformed into high-viscous liquid crystalline phases at the injection site. Ternary phase diagrams were constructed from various triglycerides: sesame oil, soybean oil and olive oil. In this study, monoglyceride-based drug delivery systems were prepared in the ratio of triglycerides: monoglyceride: water as 8: 62: 30 and 12: 58: 30. These systems could sustain release of Garcinia Mangostana husk extract over a period of 48 hr and followed squared root of time kinetics during the initial 24 hr of the release phase, indicating that the rate of release was diffusion-controlled. The system containing sesame oil showed the highest drug release. The increasing triglyceride content did not affect the release profiles. Differential scanning calorimetry results demonstrated that Garcinia Mangostana husk extract could be incorporated into drug delivery systems without causing phase transition. In the in vitro test, monoglyceride-based drug delivery systems containing Garcinia mangostana husk extract did not show the antimicrobial activity probably due to the high lipophilicity of the extract therefore it did not diffuse into the medium. Additionally, the drug delivery systems containing Garcinia mangostana husk extract showed good stability under the stress condition.
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Yaron, Zvi, Abigail Elizur, Martin Schreibman, and Yonathan Zohar. Advancing Puberty in the Black Carp (Mylopharyngodon piceus) and the Striped Bass (Morone saxatilis). United States Department of Agriculture, 2000. http://dx.doi.org/10.32747/2000.7695841.bard.

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Abstract:
Both the genes and cDNA sequences encoding the b-subunits of black carp LH and FSH were isolated, cloned and sequenced. Sequence analysis of the bcFSHb and LHb5'flanking regions revealed that the promoter region of both genes contains canonical TATA sequences, 30 bp and 17 bp upstream of the transcription start site of FSHb and LHb genes, respectively. In addition, they include several sequences of cis-acting motifs, required for inducible and tissue-specific transcriptional regulation: the gonadotropin-specific element (GSE), GnRH responsive element (GRE), half sites of estrogen and androgen response elements, cAMP response element, and AP1. Several methods have been employed by the Israeli team to purify the recombinant b subunits (EtOH precipitation, gel filtration and lentil lectin). While the final objective to produce pure recombinantGtH subunits has not yet been achieved, we have covered much ground towards this goal. The black carp ovary showed a gradual increase in both mass and oocyte diameter. First postvitellogenic oocytes were found in 5 yr old fish. At this age, the testes already contained spermatozoa. The circulating LH levels increased from 0.5 ng/ml in 4 yr old fish to &gt;5ng/ml in 5 yr old fish. In vivo challenge experiments in black carp showed the initial LH response of the pituitary to GnRH in 4 yr old fish. The response was further augmented in 5 yr old fish. The increase in estradiol level in response to gonadotropic stimulation was first noted in 4 yr old fish but this response was much stronger in the following year. In vivo experiments on the FSHb and LHb mRNA levels in response to GnRH were carried out on common carp as a model for synchronom spawning cyprinids. These experiments showed the prevalence of FSHP in maturing fish while LHP mRNA was prevalent in mature fish, especially in females. The gonadal fat-pad was found to originate from the retroperitoneal mesoderm and not from the genital ridge, thus differing from that reported in certain amphibians This tissue possibly serves as the major source of sex steroids in the immature black carp. However, such a function is taken over by the developing gonads in 4 yr old fish. In the striped bass, we described the ontogeny of the neuro-endocrine parameters along the brain-pituitary-gonadal axis during the first four years of life, throughout gonadal development and the onset of puberty. We also described the responsiveness of the reproductive axis to long-term hormonal manipulations at various stages of gonadal development. Most males reached complete sexual maturity during the first year of life. Puberty was initiated during the third year of life in most females, but this first reproductive cycle did not lead to the acquisition of full sexual maturity. This finding indicates that more than one reproductive cycle may be required before adulthood is reached. Out of the three native GnRHs present in striped bass, only sbGnRH and cGnRH II increased concomitantly with the progress of gonadal development and the onset of puberty. This finding, together with data on GtH synthesis and release, suggests that while sbGnRH and cGnRH II may be involved in the regulation of puberty in striped bass, these neuropeptides are not limiting factors to the onset of puberty. Plasma LH levels remained low in all fish, suggesting that LH plays only a minor role in early gonadal development. This hypothesis was further supported by the finding that experimentally elevated plasma LH levels did not result in the induction of complete ovarian and testicular development. The acquisition of complete puberty in 4 yr old females was associated with a rise in the mRNA levels of all GtH subunit genes, including a 218-fold increase in the mRNA levels of bFSH. mRNA levels of the a and PLH subunits increased only 11- and 8-fold, respectively. Although data on plasma FSH levels are unavailable, the dramatic increase in bFSH mRNA suggests a pivotal role for this hormone in regulating the onset and completion of puberty in striped bass. The hormonal regulation of the onset of puberty and of GtH synthesis and release was studied by chronic administration of testosterone (T) and/or an analog of gonadotropin-releasing hormone (G). Sustained administration of T+G increased the mRNA levels of the PLH subunit to the values characteristic of sexually mature fish, and also increased the plasma levels of LH. However, these changes did not result in the acceleration of sexual maturation. The mRNA levels of the bFSH subunit were slightly stimulated, but remained about 1/10 of the values characteristic of sexually mature fish. It is concluded that the stimulation of FSH gene expression and release does not lead to the acceleration of sexual maturity, and that the failure to sufficiently stimulate the bFSH subunit gene expression may underlie the inability of the treatments to advance sexual maturity. Consequently, FSH is suggested to be the key hormone to the initiation and completion of puberty in striped bass. Future efforts to induce precocious puberty in striped bass should focus on understanding the regulation of FSH synthesis and release and on developing technologies to induce these processes. Definite formulation of hormonal manipulation to advance puberty in the striped bass and the black carp seems to be premature at this stage. However, the project has already yielded a great number of experimental tools of DNA technology, slow-release systems and endocrine information on the process of puberty. These systems and certain protocols have been already utilized successfully to advance maturation in other fish (e.g. grey mullet) and will form a base for further study on fish puberty.
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